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α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
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Oral Hypoglycemic Agents: Sulfonylureas01:17

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A Mouse Model of Hemorrhagic Transformation Induced by Acute Hyperglycemia Combined with Transient Focal Ischemia
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Human Data Supporting Glyburide in Ischemic Stroke.

Kevin N Sheth1, J Marc Simard2, Jordan Elm3

  • 1Division of Neurocritical Care and Emergency Neurology, Yale University School of Medicine, 15 York Street, LCI 10th Floor, New Haven, CT, 06520, USA. kevin.sheth@yale.edu.

Acta Neurochirurgica. Supplement
|October 15, 2015
PubMed
Summary
This summary is machine-generated.

Glyburide, a SUR1-TRPM4 channel blocker, shows promise in treating ischemic stroke by reducing brain swelling and improving patient outcomes. Further studies are needed to confirm its efficacy as a stroke pharmacotherapy.

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Cardiovascular Research

Background:

  • The SUR1-TRPM4 channel plays a key role in brain edema and hemorrhagic transformation following focal ischemia.
  • Glyburide, a small molecule inhibitor of this channel, has demonstrated neuroprotective effects in preclinical models of ischemic stroke.

Purpose of the Study:

  • To evaluate the safety and potential efficacy of intravenous glyburide (RP-1127) in patients with ischemic stroke.
  • To assess RP-1127's ability to reduce brain swelling and hemorrhagic transformation.

Main Methods:

  • Retrospective analysis of diabetic stroke patients on sulfonylureas.
  • Early phase II study utilizing magnetic resonance imaging and plasma biomarkers.
  • Ongoing phase II clinical trial assessing safety, feasibility, and tolerability.

Main Results:

  • Preclinical models show improved survival and neurological outcomes with glyburide.
  • Retrospective data suggest better outcomes for stroke patients continuing sulfonylureas.
  • Phase II data indicate RP-1127 may decrease swelling and hemorrhagic transformation.

Conclusions:

  • Intravenous glyburide (RP-1127) presents a potential therapeutic option for severe stroke patients.
  • Continued clinical development, including definitive efficacy studies, is warranted.
  • RP-1127 has demonstrated safety, feasibility, and tolerability in ongoing trials.